JP2019524646A5

JP2019524646A5 -

Info

Publication number: JP2019524646A5
Application number: JP2018562323A
Authority: JP
Filing date: 2017-06-29
Publication date: 2020-08-06
Anticipated expiration: 2037-06-29

Description

この例において、有効成分は、本発明にかかる化合物のいずれかの同じ量と、とりわけ、例証された化合物のいずれかの同じ量と取り替えることが可能である。
本発明は以下の態様を含みうる。
［１］式（Ｉ）の化合物、その互変異性体又は立体異性型、並びに薬学的に許容可能な付加塩及び溶媒和物であって、

式中、
Ｒ ^１はＣ _１−４アルキルを表わし；
Ｒ ^２は、Ｃ _１−６アルキル、１つのＲ ^５で置換されたＣ _１−６アルキル、又は１、２、或いは３つのフルオロ原子で置換されたＣ _１−６アルキルを表わし；
ＹはＣＲ ^４又はＮを表わし；
Ｒ ^４は水素又はハロを表わし；
Ｒ ^５は、Ｈｅｔ ^３ａ、−ＮＲ ^６ａＲ ^６ｂ、又は−ＯＲ ^７を表わし；
Ｒ ^６ａは水素又はＣ _１−４アルキルを表わし；
Ｒ ^６ｂは水素；Ｃ _１−４アルキル；Ｃ _３−６シクロアルキル；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｈｅｔ ^４；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；−ＯＨ及び−ＮＲ ^１６ａＲ ^１６ｂから成る群から選択される１つの置換基で置換される−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；又は−ＯＨ及び−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルを表わし；
Ｒ ^７は水素、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−ＮＲ ^８ａＲ ^８ｂ、−Ｃ（＝Ｏ）−Ｒ ^９、−Ｓ（＝Ｏ） _２ −ＯＨ、−Ｐ（＝Ｏ） _２ −ＯＨ、−（Ｃ＝Ｏ）−ＣＨ（ＮＨ _２）−Ｃ _１−４アルキル−Ａｒ１、又は−Ｃ _１−４アルキル−Ｈｅｔ ^３ｂを表わし；
Ｒ ^８ａは水素又はＣ _１−４アルキルを表わし；
Ｒ ^８ｂは水素、Ｃ _１−４アルキル、又はＣ _３−６シクロアルキルを表わし；
Ｒ ^９はＣ _１−６アルキル、又は、−ＮＨ _２、−ＣＯＯＨ、及びＨｅｔ ^６から成る群から選択される１つの置換基で置換されるＣ _１−６アルキルを表わし；
Ｒ ^１６ａとＲ ^１６ｂはそれぞれ独立して、水素、Ｃ _１−４アルキル、又はＣ _３−６シクロアルキルを表わし；
Ｒ ^３は、
ａ）式（１ａ−１）又は（１ａ−２）の縮合二環式環系を表わし：

環Ａ１は、１又は２つのＮ原子を含む６員芳香族複素環を表わし；
環Ａ２は、２−オキソ−１，２−ジヒドロピリジン−３−イルを表わし；
環Ｂ１は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の飽和ヘテロシクリルを表わし；
ここで、（１ａ−１）及び（１ａ−２）は、ハロ；シアノ；オキソ；−ＯＨ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ａ）−Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換される−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；Ｃ _３−６シクロアルキル；−Ｏ−Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；−Ｏ−Ｈｅｔ ^１ｂ；Ｒ ^１８；−Ｐ（＝Ｏ）−（Ｃ _１−４アルキル） _２；−ＮＨ−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−ＮＨ−Ｃ（＝Ｏ）−Ｈｅｔ ^１ｇ；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；
ここで、環Ａ２は、可能な場合、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群から選択される置換基で、Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８が環Ａ２のＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとし；及び
ここで、環Ｂ１は、可能な場合、Ｃ _１−６シクロアルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌ；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８が環Ｂ１のＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとし；又は
Ｒ ^３は、
ｂ）式（２ａ−１）の縮合二環式環系を表わし：

環Ａは、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−Ｏ−Ｃ _１−４アルキル、及び１、２、又は３つのハロ原子で置換されるＣ _１−４アルキルから成る群から選択される１つの置換基で随意に置換されるピラゾリルを表わし；
環Ｂは、Ｃ _５−７シクロアルキル、又は、Ｏ及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む５〜７員の飽和ヘテロシクリルを表わし；
ここで、前記Ｃ _５−７シクロアルキル又は５〜７員の飽和ヘテロシクリルは、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−Ｏ−Ｃ _１−４アルキル、及び−Ｃ _１−４アルキル−ＯＨから成る群からそれぞれ独立して選択される１又は２つの置換基で、１又は２つの環炭素原子上で随意に置換される場合があり、或いは、１つの環炭素原子はオキソで随意に置換される場合があり；及び
ここで、前記５〜７員の飽和ヘテロシクリルは、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；又は
Ｒ ^３は、
ｃ）Ｏ、Ｓ、及びＮからそれぞれ独立して選択される、１又は２つのヘテロ原子を含有する６〜１１員の二環式芳香族複素環系を表わし；
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、ハロ；シアノ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ａ）−Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換される−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；Ｃ _３−６シクロアルキル；−Ｏ−Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；−Ｏ−Ｈｅｔ ^１ｂ；Ｒ ^１８；−Ｐ（＝Ｏ）−（Ｃ _１−４アルキル） _２；−ＮＨ−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−ＮＨ−Ｃ（＝Ｏ）−Ｈｅｔ ^１ｇ；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、可能な場合、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌ；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群から選択される置換基で、１つの環Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８がＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとし；
Ｒ ^１０は−ＯＨ、−Ｏ−Ｃ _１−４アルキル、−ＮＲ ^１１ａＲ ^１１ｂ、又はＨｅｔ ^２を表わし；
Ｒ ^１８は、１、２、又は３つのＮ原子を含む５員芳香環を表わし；
ここで、前記５員芳香環は、Ｃ _１−４アルキル及びＣ _３−６シクロアルキルから成る群から選択される１つの置換基で随意に置換される場合があり；
Ｈｅｔ ^１ａ、Ｈｅｔ ^１ｃ、及びＨｅｔ ^１ｄはそれぞれ独立して、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の単環式飽和ヘテロシクリル；又は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１、２、又は３つのヘテロ原子を含む、縮合環、スピロ環、及び架橋環を含む６〜１１員の二環式飽和ヘテロシクリルを表わし；
ここで、前記４〜７員の単環式飽和ヘテロシクリル、又は前記６〜１１員の二環式飽和ヘテロシクリルは、可能な場合、Ｃ _１−４アルキル、Ｃ _３−６シクロアルキル、及び−ＯＨと−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルからそれぞれ独立して選択される置換基で、１、２、又は３つの環Ｎ原子上で随意に置換される場合があり；及び
ここで、前記４〜７員の単環式飽和ヘテロシクリル、又は前記６〜１１員の二環式飽和ヘ
テロシクリルは、−ＯＨ、オキソ、ハロ、Ｃ _１−４アルキル、シアノ、−Ｃ（＝Ｏ）−Ｃ _１−４アルキル、−Ｏ−Ｃ _１−４アルキル、−ＮＨ _２、−ＮＨ（Ｃ _１−４アルキル）、及び−Ｎ（Ｃ _１−４アルキル） _２から成る群からそれぞれ独立して選択される１又は２つの置換基で、１、２、又は３つの環Ｃ原子上で随意に置換される場合があり；
Ｈｅｔ ^１ｂ、Ｈｅｔ ^１ｅ、Ｈｅｔ ^１ｇ、及びＨｅｔ ^４はそれぞれ独立して、任意の利用可能な環炭素原子を介して式（Ｉ）の分子の残部に結合される、４〜７員の単環式飽和ヘテロシクリルを表わし、前記Ｈｅｔ ^１ｂ、Ｈｅｔ ^１ｅ、Ｈｅｔ ^１ｇ、及びＨｅｔ ^４は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含有しており；
ここで、前記４〜７員の単環式飽和ヘテロシクリルは、可能な場合、Ｃ _１−４アルキル、Ｃ _３−６シクロアルキル、及び−ＯＨと−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；及び
ここで、前記４〜７員の単環式飽和ヘテロシクリルは、−ＯＨ、ハロ、Ｃ _１−４アルキル、シアノ、−Ｃ（＝Ｏ）−Ｃ _１−４アルキル、−Ｏ−Ｃ _１−４アルキル、−ＮＨ _２、−ＮＨ（Ｃ _１−４アルキル）、及び−Ｎ（Ｃ _１−４アルキル） _２から成る群からそれぞれ独立して選択される１又は２つの置換基で、１、２、又は３つの環Ｃ原子上で随意に置換される場合があり；
Ｈｅｔ ^２は、式（ｂ−１）のヘテロシクリルを表わし：

（ｂ−１）は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮから選択される１つの追加のヘテロ原子を随意に含むＮ結合の４〜７員の単環式飽和ヘテロシクリル、或いは、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つの追加のヘテロ原子を随意に含む、縮合環、スピロ環、及び架橋環を含むＮ結合の６〜１１員の二環式飽和ヘテロシクリルを表わし；
ここで、（ｂ−１）が１又は２つの追加のＮ原子を含む場合、前記１又は２つのＮ原子はＣ _１−４アルキルで随意に置換される場合があり；及び
ここで、（ｂ−１）は、ハロ、−ＯＨ、シアノ、Ｃ _１−４アルキル、−Ｏ−Ｃ _１−４アルキル、−ＮＨ _２、−ＮＨ（Ｃ _１−４アルキル）、−Ｎ（Ｃ _１−４アルキル） _２、及びＣ _１−４アルキル−ＯＨから成る群からそれぞれ独立して選択される１又は２つの置換基で、１、２、又は３つの環Ｃ原子上で随意に置換される場合があり；
Ｒ ^１１ｂは水素；Ｈｅｔ ^１ｅ；Ｃ _１−４アルキル；Ｃ _１−４アルキル−Ｈｅｔ ^５；ハロ、−ＯＨ、及び−Ｏ−Ｃ _１−４アルキルから成る群からそれぞれ独立して選択される１、２、又は３つの置換基で置換されるＣ _１−４アルキル；Ｃ _３−６シクロアルキル；又はハロ、−ＯＨ、及び−Ｏ−Ｃ _１−４アルキルから成る群からそれぞれ独立して選択される１、２、又は３つの置換基で置換されるＣ _３−６シクロアルキルを表わし；
Ｒ ^１３は、−Ｏ−Ｃ _１−４アルキル、−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂ、−ＮＲ ^１９ａＲ ^１９ｂ、Ｃ _３−６シクロアルキル、Ｈｅｔ ^１ｄ、−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル、−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ｃ）−Ｃ _１−４アルキル、又は−Ｃ（＝Ｏ）−Ｈｅｔ ^１ｆを表わし；
Ｒ ^１２は−ＯＨ、−Ｏ−Ｃ _１−４アルキル、−ＮＲ ^１４ａＲ ^１４ｂ、−Ｃ（＝Ｏ）ＮＲ ^１４ｃＲ ^１４ｄ、−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル、−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ｂ）−Ｃ _１−４アルキル、Ｃ _３−６シクロアルキル、Ａｒ ^２、又はＨｅｔ ^１ｃを表わし；
Ａｒ ^１は１つのヒドロキシで随意に置換されるフェニルを表わし；
Ａｒ ^２は１つのＣ _１−４アルキルで随意に置換されるフェニルを表わし；
Ｈｅｔ ^３ａ、Ｈｅｔ ^３ｂ、Ｈｅｔ ^５、Ｈｅｔ ^６、及びＨｅｔ ^１ｆはそれぞれ独立して式（ｃ−１）のヘテロシクリルを表わし：

（ｃ−１）は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮから選択される１つの追加のヘテロ原子を随意に含むＮ結合の４〜７員の単環式飽和ヘテロシクリルを表わし；
ここで、（ｃ−１）が１つの追加のＮ原子を含む場合、追加のＮ原子はＣ _１−４アルキル又はＣ _３−６シクロアルキルで随意に置換される場合があり；及び
ここで、（ｃ−１）は、ハロ、Ｃ _１−４アルキル、及びＣ _３−６シクロアルキルから成る群からそれぞれ独立して選択される１又は２つの置換基で、１又は２つの環Ｃ原子上で随意に置換される場合があり；
Ｒ ^１１ａ、Ｒ ^１４ａ、Ｒ ^１４ｃ、Ｒ ^１４ｇ、Ｒ ^１４ｉ、Ｒ ^１４ｋ、Ｒ ^１５ａ、Ｒ ^１７ａ、及びＲ ^１９ａはそれぞれ独立して、水素又はＣ _１−４アルキルを表わし；
Ｒ ^１４ｂ、Ｒ ^１４ｄ、Ｒ ^１４ｈ、Ｒ ^１４ｊ、Ｒ ^１４ｌ、Ｒ ^１５ｂ、Ｒ ^１７ｂ、及びＲ ^１９ｂはそれぞれ独立して、水素；Ｃ _１−４アルキル；Ｃ _３−６シクロアルキル；又は、ハロ、−ＯＨ、及び−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルを表わし；
Ｒ ^２０ａ、Ｒ ^２０ｂ、及びＲ ^２０ｃはそれぞれ独立して、水素；Ｃ _１−４アルキル；Ｃ _３−６シクロアルキル；又は−ＯＨ及び−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルを表わし；
ｐは１又は２を表わす
ことを特徴とする化合物。
［２］Ｒ ^３は、式（１ａ−１）又は（１ａ−２）の縮合二環式環系を表わし：

環Ａ１は、１又は２つのＮ原子を含む６員芳香族複素環を表わし；
環Ａ２は、２−オキソ−１，２−ジヒドロピリジン−３−イルを表わし；
環Ｂ１は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の飽和ヘテロシクリルを表わし；
ここで、（１ａ−１）及び（１ａ−２）は、ハロ；シアノ；オキソ；−ＯＨ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ａ）−Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換される−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；Ｃ _３−６シクロアルキル；−Ｏ−Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；−Ｏ−Ｈｅｔ ^１ｂ；Ｒ ^１８；−Ｐ（＝Ｏ）−（Ｃ _１−４アルキル） _２；−ＮＨ−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−ＮＨ−Ｃ（＝Ｏ）−Ｈｅｔ ^１ｇ；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；
ここで、環Ａ２は、可能な場合、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群から選択される置換基で、Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８が環Ａ２のＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとし；及び
ここで、環Ｂ１は、可能な場合、Ｃ _１−６シクロアルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌ；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８が環Ｂ１のＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとする
ことを特徴とする上記［１］に記載の化合物。
［３］Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−ＮＲ ^８ａＲ ^８ｂ、−Ｃ（＝Ｏ）−Ｒ ^９、−（Ｃ＝Ｏ）−ＣＨ（ＮＨ _２）−、又はＣ _１−４アルキル−Ａｒ ^１を表わし；
Ｒ ^９はＣ _１−６アルキル、又は、−ＮＨ _２及び−ＣＯＯＨから成る群から選択される１つの置換基で置換されるＣ _１−６アルキルを表わし；
Ｒ ^３は、式（１ａ−１）の縮合二環式環系を表わし：

環Ａ１は、１又は２つのＮ原子を含む６員芳香族複素環を表わし；
環Ｂ１は、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の飽和ヘテロシクリルを表わし；
ここで、（１ａ−１）は、ハロ；シアノ；オキソ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換される−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；Ｃ _３−６シクロアルキル；−Ｏ−Ｃ _３−６シクロアルキル；−ＮＨ−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、環Ｂ１は、可能な場合、Ｃ _１−６シクロアルキル；Ｃ _３−６シクロアルキル；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌ；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；
Ｒ ^１０は−ＯＨ、−Ｏ−Ｃ _１−４アルキル、又は−ＮＲ ^１１ａＲ ^１１ｂを表わし；
Ｒ ^１１ｂは水素；Ｃ _１−４アルキル；ハロ、−ＯＨ、及び−Ｏ−Ｃ _１−４アルキルから成る群からそれぞれ独立して選択される１、２、又は３つの置換基で置換されるＣ _１−４アルキル；Ｃ _３−６シクロアルキル；又はハロ、−ＯＨ、及び−Ｏ−Ｃ _１−４アルキルから成る群からそれぞれ独立して選択される１、２、又は３つの置換基で置換されるＣ _３−６シクロアルキルを表わし；
Ｒ ^１３は−Ｏ−Ｃ _１−４アルキル、−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂ、−ＮＲ ^１９ａＲ ^１９ｂ、Ｃ _３−６シクロアルキル、又は−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキルを表わし；
Ｒ ^１２は−ＯＨ、−Ｏ−Ｃ _１−４アルキル、−ＮＲ ^１４ａＲ ^１４ｂ、−Ｃ（＝Ｏ）ＮＲ ^１４ｃＲ ^１４ｄ、−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル、Ｃ _３−６シクロアルキル、又はＡｒ ^２を表わす
ことを特徴とする上記［１］又は［２］に記載の化合物。
［４］Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、式（１ａ−１）の縮合二環式環系を表わし：

環Ａ１は、１又は２つのＮ原子を含む６員芳香族複素環を表わし；
環Ｂ１は、Ｏ及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の飽和ヘテロシクリルを表わし；
ここで、（１ａ−１）は、ハロ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、環Ｂ１は、可能な場合、Ｃ _１−６シクロアルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；及び−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；
Ｒ ^１０は−ＮＲ ^１１ａＲ ^１１ｂを表わし；
Ｒ ^１１ｂはＣ _１−４アルキルを表わし；
Ｒ ^１３は−Ｏ−Ｃ _１−４アルキル、−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂ、又はＣ _３−６シクロアルキルを表わし；
Ｒ ^１２はＣ _３−６シクロアルキルを表わし；
Ｒ ^１１ａ、Ｒ ^１４ｉ、Ｒ ^１４ｋ、Ｒ ^１５ａ、及びＲ ^１７ａはそれぞれ独立して、水素又はＣ _１−４アルキルを表わし；
Ｒ ^１４ｊ、Ｒ ^１４ｌ、Ｒ ^１５ｂ、及びＲ ^１７ｂはそれぞれ独立して、水素又はＣ _１−４アルキルを表わす
ことを特徴とする上記［１］又は［２］に記載の化合物。
［５］Ｒ ^２は、１つのＲ ^５で置換されるＣ _１−６アルキルを表わし；
Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、式（１ａ−１）の縮合二環式環系を表わし：

環Ａ１は、フェニル、又は１つのＮ原子を含む６員芳香族複素環を表わし；
環Ｂ１は、Ｏ及びＮから選択される１つのヘテロ原子を含む４〜７員の飽和ヘテロシクリルを表わし；
ここで、（１ａ−１）は、−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；及び１つのＲ ^１３で置換されるＣ _１−４アルキルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、環Ｂは、可能な場合、Ｃ _１−６アルキル置換基で、１つのＮ原子上で随意に置換される場合があり；
Ｒ ^１３はＣ _３−６シクロアルキルを表わし；
Ｒ ^１２はＣ _３−６シクロアルキルを表わす
ことを特徴とする上記［１］又は［２］に記載の化合物。
［６］Ｒ ^３は、式（２ａ−１）の縮合二環式環系を表わし：

環Ａは、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−Ｏ−Ｃ _１−４アルキル、及び１、２、又は３つのハロ原子で置換されるＣ _１−４アルキルから成る群から選択される１つの置換基で随意に置換されるピラゾリルを表わし；
環Ｂは、Ｃ _５−７シクロアルキル、又は、Ｏ及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む５〜７員の飽和ヘテロシクリルを表わし；
ここで、前記Ｃ _５−７シクロアルキル又は５〜７員の飽和ヘテロシクリルは、Ｃ _１−４アルキル、−Ｃ _１−４アルキル−Ｏ−Ｃ _１−４アルキル、及び−Ｃ _１−４アルキル−ＯＨから成る群からそれぞれ独立して選択される１又は２つの置換基で、１又は２つの環炭素原子上で随意に置換される場合があり、或いは、１つの環炭素原子はオキソで随意に置換される場合があり；及び
ここで、前記５〜７員の飽和ヘテロシクリルは、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合がある
ことを特徴とする上記［１］に記載の化合物。
［７］Ｒ ^１はＣ _１−４アルキルを表わし；
Ｒ ^２は、１つのＲ ^５で置換されるＣ _１−６アルキルを表わし；
Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、式（２ａ−１）の縮合二環式環系を表わし：

環Ａは、Ｃ _１−４アルキル、及び−Ｃ _１−４アルキル−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で随意にされるピラゾリルを表わし；
環Ｂは、Ｃ _５−７シクロアルキル、又は、Ｏ及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む５〜７員の飽和ヘテロシクリルを表わし；
ここで、前記Ｃ _５−７シクロアルキル又は５〜７員の飽和ヘテロシクリルは、１又は２つのＣ _１−４アルキル置換基で、１つの環炭素原子上で随意に置換される場合があり、又は１つの環炭素原子はオキソで随意に置換される場合があり；及び
ここで、前記５〜７員の飽和ヘテロシクリルは、Ｃ _１−６アルキル置換基で、１又は２つの環Ｎ原子上で随意に置換される場合がある
ことを特徴とする上記［６］に記載の化合物。
［８］Ｒ ^１はＣ _１−４アルキルを表わし；
Ｒ ^２は、１つのＲ ^５で置換されるＣ _１−６アルキルを表わし；
Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、式（２ａ−１）の縮合二環式環系を表わし：

環Ａはピラゾリルを表わし；
環Ｂは、Ｏ及びＮから選択される１つのヘテロ原子を含む６員飽和ヘテロシクリルを表わし；
ここで、前記６員飽和ヘテロシクリルは、１つのＣ _１−４アルキル置換基で、１つの環炭素原子上で随意に置換される場合があり、１つの環炭素原子はオキソで随意に置換される場合があり；及び
ここで、前記５〜７員の飽和ヘテロシクリルは、Ｃ _１−６アルキル置換基で、１つのＮ原子上で随意に置換される場合がある
ことを特徴とする上記［６］に記載の化合物。
［９］Ｒ ^３は、以下の構造から選択される縮合二環式環系を表わす

ことを特徴とする上記［８］に記載の化合物。
［１０］Ｒ ^３は、Ｏ、Ｓ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含有する、縮合した６〜１１員の二環式芳香族複素環系を表わし；
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、ハロ；シアノ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）−Ｒ ^１０；−Ｓ（＝Ｏ） _２ −Ｃ _１−４アルキル；−Ｓ（＝Ｏ）（＝Ｎ−Ｒ ^２０ａ）−Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換される−Ｏ−Ｃ _１−４アルキル；−Ｏ−Ｃ _１−４アルキル−Ｒ ^１２；Ｃ _３−６シクロアルキル；−Ｏ−Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；−Ｏ−Ｈｅｔ ^１ｂ；Ｒ ^１８；−Ｐ（＝Ｏ）−（Ｃ _１−４アルキル） _２；−ＮＨ−Ｃ（＝Ｏ）−Ｃ _１−４アルキル；−ＮＨ−Ｃ（＝Ｏ）−Ｈｅｔ ^１ｇ；−ＮＲ ^１７ａＲ ^１７ｂ；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、可能な場合、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；Ｈｅｔ ^１ａ；Ｒ ^１８；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；−（Ｃ＝Ｏ）−Ｃ _１−４アルキル；−Ｃ（＝Ｏ）ＮＲ ^１４ｇＲ ^１４ｈ；−Ｃ（＝Ｏ）−Ｃ _１−４アルキル−ＮＲ ^１４ｉＲ ^１４ｊ；−Ｃ（＝Ｏ）−Ｃ（＝Ｏ）−ＮＲ ^１４ｋＲ ^１４ｌ；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群から選択される置換基で、１つの環Ｎ原子上で随意に置換される場合があり；但し、Ｈｅｔ ^１ａ又はＲ ^１８がＮ原子に直接結合される場合、前記Ｈｅｔ ^１ａ又はＲ ^１８は環炭素原子を介してＮ原子に結合されるものとする
ことを特徴とする上記［１］に記載の化合物。
［１１］Ｒ ^５は、−ＮＲ ^６ａＲ ^６ｂ又は−ＯＲ ^７を表わし；
Ｒ ^６ｂは水素；Ｃ _１−４アルキル；Ｃ _３−６シクロアルキル；又は−Ｃ（＝Ｏ）−Ｃ _１−４アルキルを表わし；
Ｒ ^７は水素、Ｃ _１−４アルキル、又は−Ｃ _１−４アルキル−ＮＲ ^８ａＲ ^８ｂを表わし；
Ｒ ^３は、Ｏ、Ｓ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含有する、縮合した６〜１１員の二環式芳香族複素環系を表わし；
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、ハロ；シアノ；Ｃ _１−６アルキル；−Ｏ−Ｃ _１−４アルキル；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群からそれぞれ独立して選択される合計１、２、又は３つの置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、可能な場合、Ｃ _１−６アルキル；Ｃ _３−６シクロアルキル；１、２、又は３つのハロ原子で置換されるＣ _１−４アルキル；１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキル；１つのＲ ^１８で置換されるＣ _１−４アルキル；Ｃ _２−６アルケニル；及び１つのＲ ^１３で置換されるＣ _２−６アルケニルから成る群から選択される置換基で、１つの環Ｎ原子上で随意に置換される場合があり；
Ｈｅｔ ^１ｄは、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の単環式飽和ヘテロシクリルを表わし；
ここで、前記４〜７員の単環式飽和ヘテロシクリルは、可能な場合、Ｃ _１−４アルキル、Ｃ _３−６シクロアルキル、及び−ＯＨと−Ｏ−Ｃ _１−４アルキルから成る群から選択される１つの置換基で置換されるＣ _１−４アルキルから成る群からそれぞれ独立して選択される置換基で、１又は２つの環Ｎ原子上で随意に置換される場合があり；及び
ここで、前記４〜７員の単環式飽和ヘテロシクリルは、−ＯＨ、ハロ、Ｃ _１−４アルキル、シアノ、−Ｏ−Ｃ _１−４アルキル、−ＮＨ _２、−ＮＨ（Ｃ _１−４アルキル）、及び−Ｎ（Ｃ _１−４アルキル） _２から成る群からそれぞれ独立して選択される１又は２つの置換基で、１、２、又は３つの環Ｃ原子上で随意に置換される場合があり；
Ｒ ^１３は−Ｏ−Ｃ _１−４アルキル、−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂ、−ＮＲ ^１９ａＲ ^１９ｂ、Ｃ _３−６シクロアルキル、又はＨｅｔ ^１ｄを表わす
ことを特徴とする上記［１０］に記載の化合物。
［１２］Ｒ ^１はＣ _１−４アルキルを表わし；
Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、Ｏ、Ｓ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含有する、縮合した６〜１１員の二環式芳香族複素環系を表わし；
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、合計１、２、又は３つのハロ置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、可能な場合、１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキルから成る群から選択される置換基で、１つの環Ｎ原子上で随意に置換される場合があり；
Ｈｅｔ ^１ｄは、Ｏ、Ｓ、Ｓ（＝Ｏ） _ｐ、及びＮからそれぞれ独立して選択される１又は２つのヘテロ原子を含む４〜７員の単環式飽和ヘテロシクリルを表わし；
Ｒ ^１３は−Ｏ−Ｃ _１−４アルキル、−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂ、又はＨｅｔ ^１ｄを表わし；
Ｒ ^１５ａは水素又はＣ _１−４アルキルを表わし；
Ｒ ^１５ｂはＣ _１−４アルキルを表わす
ことを特徴とする上記［１０］に記載の化合物。
［１３］Ｒ ^１はＣ _１−４アルキルを表わし；
Ｒ ^５は−ＯＲ ^７を表わし；
Ｒ ^７は水素を表わし；
Ｒ ^３は、１つのＮ原子を含む縮合した９員の二環式芳香族複素環系を表わし；
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、合計１、２、又は３つのハロ置換基で、環炭素原子上で随意に置換される場合があり；及び
ここで、前記縮合した６〜１１員の二環式芳香族複素環系は、可能な場合、１、２、又は３つの−ＯＨ置換基で置換されるＣ _１−４アルキル；１つのＲ ^１３で置換されるＣ _１−４アルキルから成る群から選択される置換基で、１つの環Ｎ原子上で随意に置換される場合があり；
Ｒ ^１３は−Ｏ−Ｃ _１−４アルキル又は−Ｃ（＝Ｏ）ＮＲ ^１５ａＲ ^１５ｂを表わし；
Ｒ ^１５ａは水素又はＣ _１−４アルキルを表わし；
Ｒ ^１５ｂはＣ _１−４アルキルを表わす
ことを特徴とする上記［１０］に記載の化合物。
［１４］Ｒ ^１はメチルを表わし；及び
Ｒ ^２はメチル又は−ＣＨ _２ −ＯＨを表わす
ことを特徴とする上記［１］乃至［１３］の何れか１つに記載の化合物。
［１５］ＹはＣＲ ^４を表わす、ことを特徴とする上記［１］乃至［１４］の何れか１つに記載の化合物。
［１６］Ｒ ^４は水素を表わす、ことを特徴とする上記［１］乃至［１５］の何れか１つに記載の化合物。
［１７］ＹはＮを表わす、ことを特徴とする上記［１］乃至［１４］の何れか１つに記載の化合物。
［１８］化合物は、化合物２１、２５、３２、３４、３５、１ｂ、２ｂ、３ｂ、１７ｂ、３ｃ、及び８ｃ、それらの互変異性体及び立体異性型、並びに薬学的に許容可能な付加塩及び溶媒和物から選択される、ことを特徴とする上記［１］に記載の化合物。
［１９］上記［１］乃至［１８］の何れか１つに記載の化合物と、薬学的に許容可能な担体又は希釈剤とを含む、医薬組成物。
［２０］薬剤として使用するための上記［１］乃至［１８］の何れか１つに記載の化合物。
［２１］癌の予防又は処置に使用するための上記［１］乃至［１８］の何れか１つに記載の化合物。
［２２］癌の予防又は処置に使用するための上記［１９］に記載の医薬組成物。
［２３］温血動物の細胞増殖性疾患を処置又は予防する方法であって、前記温血動物に、有効な量の上記［１］乃至［１８］の何れか１つに記載の化合物を投与する工程を含む、方法。 In this example, the active ingredient can be replaced with the same amount of any of the compounds according to the invention and, above all, with the same amount of any of the exemplified compounds.
The present invention may include the following aspects.
[1] a compound of formula (I), its tautomer or stereoisomeric form, and pharmaceutically acceptable addition salts and solvates,

In the formula,
R ¹ represents C _1-4 alkyl;
R ² _{is, C 1-6} represents alkyl, _{C 1-6} alkyl substituted with one ^{R 5,} or 1, 2, or _{C 1-6} alkyl substituted with 3 fluoro atoms;
Y represents CR ⁴ or N;
R ⁴ represents hydrogen or halo;
R ⁵ represents Het ^3a , —NR ^6a R ^6b , or —OR ⁷ ;
R ^6a represents hydrogen or C _1-4 alkyl;
R ^6b is hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; -C(=O)-C _1-4 alkyl; -C(=O)-Het ⁴ ; -S(=O) ₂ -C. _1-4 alkyl; -OH and -NR ^16a R ^16b, -C(=O)-C _1-4 alkyl substituted with one substituent selected from the group consisting of : -OH and -S(=O ) Represents C _1-4 alkyl substituted with one substituent selected from the group consisting of _2- C _1-4 alkyl ;
R ⁷ is _{hydrogen, C 1-4} _{alkyl, -C 1-4} alkyl ^{^{^{-NR 8a R 8b, -C (=}}} O) -R 9, -S (= O) 2 -OH, -P (= O) 2 -OH, - (C = O) -CH (NH 2) -C 1-4 alkyl -Ar1, or _{-C 1-4} alkyl -Het ^3b;
R ^8a represents hydrogen or C _1-4 alkyl;
R ^8b represents hydrogen, C _1-4 alkyl, or C _3-6 cycloalkyl;
R ⁹ is _{C 1-6} alkyl, _or, -NH 2, -COOH, and _{C 1-6} alkyl substituted with one substituent selected from the group consisting of Het ⁶ represents;
R ^16a and R ^16b each independently represent hydrogen, C _1-4 alkyl, or C _3-6 cycloalkyl;
R ³ is
a) represents a fused bicyclic ring system of formula (1a-1) or (1a-2):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring A2 represents 2-oxo-1,2-dihydropyridin-3-yl;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) and (1a-2) is halo, cyano, oxo; _{-OH; C 1-6} alkyl; _{-O-C 1-4} ^{alkyl; -C (= O) -R 10} ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents;
Where Ring A2 is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2 or 3 C _1-4 alkyl substituted with 3 halo atoms, where possible ; 1 , 2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2;} _{C 1-4} alkyl substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13} in and one _{C 2-6} substituents selected from the group consisting of alkenyl substituted with ^{R 13,} may be optionally substituted on the N atom; _-6 alkenyl However, ^{Het 1a} or ^{R 18} is When directly attached to the N atom of ring A2 said Het ^1a or R ¹⁸ shall be attached to the N atom via a ring carbon atom; and
Wherein Ring B1 is C _1-6 cycloalkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms, if possible ; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 18;;} _{C 1-4} alkyl substituted with one ^{R 13} - (C=O)-C _1-4 alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C( ═O)—NR ^14k R ^14l ; C _2-6 alkenyl; and substituents independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ and one or two rings N. It may be optionally substituted on an atom; provided that when Het ^1a or R ¹⁸ is directly attached to the N atom of ring B1, said Het ^1a or R ¹⁸ is attached to the N atom via a ring carbon atom. Shall; or
R ³ is
b) represents a fused bicyclic ring system of formula (2a-1):

Ring A _is selected from the group consisting of _{C 1-4} _{alkyl, -C 1-4} alkyl _{-O-C 1-4} alkyl, and 1,2, or _{C 1-4} alkyl substituted with three halo atoms Represents pyrazolyl optionally substituted with one substituent;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, the C _5-7 cycloalkyl or the 5-7 membered saturated heterocyclyl is C _1-4 alkyl, —C _1-4 alkyl-O—C _1-4 alkyl, and —C _1-4 alkyl-OH. Optionally substituted on one or two ring carbon atoms with one or two substituents each independently selected from the group consisting of, or one ring carbon atom optionally substituted with oxo. May be done; and
Wherein the 5-7 membered saturated heterocyclyl is C _1-6 alkyl; C _3-6 cycloalkyl; 1, 2 or C _1-4 alkyl substituted with 3 halo atoms ; 1, 2, or _{C 1-4} alkyl substituted with one ^{_{R 13 ;-( C = O) -C}} 1-4 alkyl;; _{C 1-4} alkyl substituted with three -OH substituents -C (= O) NR ^14g R ^14h ; optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j. In some cases; or
R ³ is
c) represents a 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S, and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents; and
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system, where possible, is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2, or 3 one of _{C 1-4} alkyl is substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; one; _{C 1-4} alkyl substituted with one ^{R 13} C _1-4 alkyl substituted with R ¹⁸ ; -( C=O)-C _1-4 alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR. ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; and a substituent selected from the group consisting of C _2-6 alkenyl substituted with one R ^13. A group may be optionally substituted on one ring N atom; provided that Het ^1a or R ¹⁸ is directly bonded to the N atom, said Het ^1a or R ¹⁸ is N via a ring carbon atom. Shall be attached to an atom;
R ¹⁰ represents —OH, —O—C _1-4 alkyl, —NR ^11a R ^11b , or Het ² ;
R ¹⁸ represents a 5-membered aromatic ring containing 1, 2, or 3 N atoms;
Wherein the 5-membered aromatic ring may be optionally substituted with one substituent selected from the group consisting of C _1-4 alkyl and C _3-6 cycloalkyl;
Het ^1a , Het ^1c , and Het ^1d are each independently a 4- to 7-membered single or four-membered heteroatom containing 1 or 2 heteroatoms independently selected from O, S, S(═O) _p , and N A cyclic saturated heterocyclyl; or a fused ring, a spiro ring, and a bridged ring containing 1, 2, or 3 heteroatoms each independently selected from O, S, S(=O) _p , and N. Represents a 6-11 membered bicyclic saturated heterocyclyl including:
Wherein the 4 to 7 membered monocyclic saturated heterocyclyl or the 6 to 11 membered bicyclic saturated heterocyclyl is combined with C _1-4 alkyl, C _3-6 cycloalkyl, and —OH , if possible. A substituent independently selected from C _1-4 alkyl substituted with one substituent selected from the group consisting of —O—C _1-4 alkyl , 1, 2, or 3 ring N atoms. May be optionally replaced above; and
Here, the 4- to 7-membered monocyclic saturated heterocyclyl or the 6- to 11-membered bicyclic saturated heterocycle.
Heterocyclyl is, -OH, oxo, _{halo, C 1-4} alkyl, cyano, _-C (= _O) -C _1-4 alkyl, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1- 4} alkyl), and —N(C _1-4 alkyl) ₂ each independently substituted with 1 or 2 substituents selected on the 1, 2 or 3 ring C atoms. May be;
Het ^1b , Het ^1e , Het ^1g , and Het ⁴ are each independently a 4-7 membered monocyclic group attached to the rest of the molecule of formula (I) through any available ring carbon atom. Represents saturated heterocyclyl, said Het ^1b , Het ^1e , Het ^1g , and Het ⁴ contain 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N. Are;
Wherein the 4-7 membered monocyclic saturated heterocyclyl is selected from the group consisting of C _1-4 alkyl, C _3-6 cycloalkyl, and —OH and —O—C _1-4 alkyl, if possible. Optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _1-4 alkyl substituted with one substituent;
Here, the 4- to 7-membered monocyclic saturated heterocyclyl is -OH, halo, C _1-4 alkyl, cyano, -C(=O)-C _1-4 alkyl, -O-C _1-4 alkyl. , —NH ₂ , —NH(C _1-4 alkyl), and —N(C _1-4 alkyl) ₂ each independently having 1 or 2 substituents, 1, 2, or It may be optionally substituted on three ring C atoms;
Het ² represents a heterocyclyl of formula (b-1):

(B-1) is an N-bonded 4-7 membered monocyclic saturated heterocyclyl optionally containing one additional heteroatom selected from O, S, S(═O) _p , and N, or 6 to 6 N-bonds, including fused, spiro, and bridged rings, optionally containing 1 or 2 additional heteroatoms each independently selected from O, S, S(=O) _p , and N. Represents an 11-membered bicyclic saturated heterocyclyl;
Where (b-1) contains 1 or 2 additional N atoms, said 1 or 2 N atoms may be optionally substituted by C _1-4 alkyl; and
Here, (b-1) is halo, -OH, _{cyano, C 1-4} alkyl, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1-4} alkyl), - N (C _1-4 alkyl) ₂ , and 1 or 2 substituents each independently selected from the group consisting of C _1-4 alkyl-OH, optionally substituted on 1, 2, or 3 ring C atoms. May be;
R ^11b is hydrogen; Het ^1e ; C _1-4 alkyl; C _1-4 alkyl- Het ⁵ ; halo, —OH, and —O—C _1-4 alkyl each independently selected from the group consisting of 1, 2, or 3 _{C 1-4} alkyl substituted with a _substituent; each independently selected from or halo, -OH, and _{-O-C 1-4} group consisting of alkyl; _{C 3-6} cycloalkyl Represents C _3-6 cycloalkyl substituted with 1, 2 or 3 substituents ;
R ¹³ is —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, Het ^1d , —S(═O) ₂ —C _{1 -4} alkyl, -S(=O)(=N-R ^20c )-C _1-4 alkyl, or -C(=O)-Het ^1f ;
R ¹² is —OH, —O—C _1-4 alkyl, —NR ^14a R ^14b , —C(═O)NR ^14c R ^14d , —S(═O) ₂ —C _1-4 alkyl, —S(= O) (=NR ^20b )-C _1-4 alkyl, C _3-6 cycloalkyl, Ar ² or Het ^1c ;
Ar ¹ represents phenyl optionally substituted with one hydroxy;
Ar ² represents phenyl optionally substituted with one C _1-4 alkyl;
Het ^3a , Het ^3b , Het ⁵ , Het ⁶ , and Het ^1f each independently represent a heterocyclyl of formula (c-1):

(C-1) represents an N-bonded 4 to 7 membered monocyclic saturated heterocyclyl optionally containing one additional heteroatom selected from O, S, S(=O) _p , and N;
Where (c-1) contains one additional N atom, the additional N atom may be optionally substituted with C _1-4 alkyl or C _3-6 cycloalkyl; and
Here, (c-1) is 1 or 2 substituents each independently selected from the group consisting of halo, C _1-4 alkyl, and C _3-6 cycloalkyl, and 1 or 2 ring C Optionally substituted on an atom;
R ^11a , R ^14a , R ^14c , R ^14g , R ¹⁴ⁱ , R ^14k , R ^15a , R ^17a , and R ^19a each independently represent hydrogen or C _1-4 alkyl;
R ^14b , R ^14d , R ^14h , R ^14j , R ^14l , R ^15b , R ^17b , and R ^19b are each independently hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or halo, -. OH, and _{-O-C 1-4} represents _{C 1-4} alkyl substituted with one substituent selected from the group consisting of alkyl;
R ^20a , R ^20b , and R ^20c are each independently selected from the group consisting of hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or —OH and —O—C _1-4 alkyl. Represents C _1-4 alkyl substituted with one substituent ;
p represents 1 or 2
A compound characterized by the following.
[2] R ³ represents a fused bicyclic ring system of formula (1a-1) or (1a-2):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring A2 represents 2-oxo-1,2-dihydropyridin-3-yl;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) and (1a-2) is halo, cyano, oxo; _{-OH; C 1-6} alkyl; _{-O-C 1-4} ^{alkyl; -C (= O) -R 10} ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents;
Where Ring A2 is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2 or 3 C _1-4 alkyl substituted with 3 halo atoms, where possible ; 1 , 2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2;} _{C 1-4} alkyl substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13} in and one _{C 2-6} substituents selected from the group consisting of alkenyl substituted with ^{R 13,} may be optionally substituted on the N atom; _-6 alkenyl However, ^{Het 1a} or ^{R 18} is When directly attached to the N atom of ring A2 said Het ^1a or R ¹⁸ shall be attached to the N atom via a ring carbon atom; and
Wherein Ring B1 is C _1-6 cycloalkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms, if possible ; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 18;;} _{C 1-4} alkyl substituted with one ^{R 13} - (C=O)-C _1-4 alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C( ═O)—NR ^14k R ^14l ; C _2-6 alkenyl; and substituents independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ and one or two rings N. It may be optionally substituted on an atom; provided that when Het ^1a or R ¹⁸ is directly attached to the N atom of ring B1, said Het ^1a or R ¹⁸ is attached to the N atom via a ring carbon atom. Shall
The compound according to the above [1], wherein
[3] R ⁵ represents -OR ⁷ ;
R ⁷ is _{hydrogen, C 1-4} _{alkyl, -C 1-4} alkyl ^{^{^{-NR 8a R 8b, -C (=}}} O) -R 9, - (C = O) -CH (NH 2) -, or _{C 1 -4} alkyl-Ar ¹ ;
R ⁹ is _{C 1-6} alkyl, or represents _{C 1-6} alkyl substituted with one substituent selected from the group consisting of -NH ₂ and -COOH;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) is halo; cyano; oxo; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S(=O) ₂ -C. _1-4 alkyl; 1,2, or _{-O-C 1-4} alkyl substituted with three halo atoms; _{-O-C 1-4} alkyl ^-R _{12; C 3-6} cycloalkyl; -O-C _3-6 _{cycloalkyl; -NH-C (= O)} -C 1-4 ^alkyl; -NR ^17a R 17b; 1,2, or _{C 1-4} alkyl is substituted with three halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R _13;} _{C 2-6} alkenyl; _{C 2-6} substituted with and one ^{R 13} Optionally substituted on a ring carbon atom with a total of 1, 2, or 3 substituents each independently selected from the group consisting of alkenyl; and
Wherein ring B1 is C _1-6 cycloalkyl; C _3-6 cycloalkyl; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms ; 1, 2, or 3 where possible. _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₃₎} _{-C 1-4} alkyl; one of _{C 1-4} alkyl substituted with -OH substituent -C (= ^{O) NR 14g} R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; and one R ^13. Optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with
R ¹⁰ represents —OH, —O—C _1-4 alkyl, or —NR ^11a R ^11b ;
R ^11b is hydrogen; C _1-4 alkyl; C substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, —OH, and —O—C _1-4 alkyl. _1-4 alkyl; C _3-6 cycloalkyl; or substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, —OH, and —O—C _1-4 alkyl. Represents C _3-6 cycloalkyl;
R ¹³ is —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, or —S(═O) ₂ —C _1-4 alkyl. Represents;
R ¹² is —OH, —O—C _1-4 alkyl, —NR ^14a R ^14b , —C(═O)NR ^14c R ^14d , —S(═O) ₂ —C _1-4 alkyl, C _3-6. Represents cycloalkyl or Ar ² .
The compound according to the above [1] or [2], characterized in that
[4] R ⁵ represents -OR ⁷ ;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, (1a-1) is halo; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -O-C _1-4 alkyl-R ¹² ;-. NR ^17a R ^17b; 1, 2, or 3 _{C 1-4} alkyl substituted with -OH substituents; _{C 1-4} alkyl substituted with one ^{R _13;} _{C 2-6} alkenyl; and one R Optionally substituted on a ring carbon atom with a total of 1, 2, or 3 substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with ¹³ ; and
Wherein ring B1 is C _1-6 cycloalkyl when possible ; C _1-4 alkyl substituted with one R ¹³ ; -( C=O)-C _1-4 alkyl; -C(=O ) -C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; and -C(=O)-C(=O)-NR ^14k R ^14l each independently have one or two substituents selected from the group consisting of: It may be optionally substituted on a ring N atom;
R ¹⁰ represents -NR ^11a R ^11b ;
R ^11b represents C _1-4 alkyl;
R ¹³ represents -O-C _1-4 alkyl, -C(=O)NR ^15a R ^15b , or C _3-6 cycloalkyl;
R ¹² represents C _3-6 cycloalkyl;
R ^11a , R ¹⁴ⁱ , R ^14k , R ^15a , and R ^17a each independently represent hydrogen or C _1-4 alkyl;
R ^14j , R ¹⁴¹ , R ^15b , and R ^17b each independently represent hydrogen or C _1-4 alkyl.
The compound according to the above [1] or [2], characterized in that
[5] R ² represents C _1-6 alkyl substituted with one R ⁵ .
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents phenyl or a 6-membered aromatic heterocycle containing one N atom;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing one heteroatom selected from O and N;
Here, (1a-1) is each a group consisting of —O—C _1-4 alkyl; —O—C _1-4 alkyl-R ¹² ; and C _1-4 alkyl substituted with one R ^13. May be optionally substituted on ring carbon atoms with a total of 1, 2 or 3 independently selected substituents; and
Wherein Ring B is optionally substituted on one N atom with a C _1-6 alkyl substituent , if possible ;
R ¹³ represents C _3-6 cycloalkyl;
R ¹² represents C _3-6 cycloalkyl
The compound according to the above [1] or [2], characterized in that
[6] R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A _is selected from the group consisting of _{C 1-4} _{alkyl, -C 1-4} alkyl _{-O-C 1-4} alkyl, and 1,2, or _{C 1-4} alkyl substituted with three halo atoms Represents pyrazolyl optionally substituted with one substituent;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, the C _5-7 cycloalkyl or the 5-7 membered saturated heterocyclyl is C _1-4 alkyl, —C _1-4 alkyl-O—C _1-4 alkyl, and —C _1-4 alkyl-OH. Optionally substituted on one or two ring carbon atoms with one or two substituents each independently selected from the group consisting of, or one ring carbon atom optionally substituted with oxo. May be done; and
Wherein the 5-7 membered saturated heterocyclyl is C _1-6 alkyl; C _3-6 cycloalkyl; 1, 2 or C _1-4 alkyl substituted with 3 halo atoms ; 1, 2, or _{C 1-4} alkyl substituted with one ^{_{R 13 ;-( C = O) -C}} 1-4 alkyl;; _{C 1-4} alkyl substituted with three -OH substituents -C (= O) NR ^14g R ^14h ; optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j. Sometimes
The compound according to the above [1], wherein
[7] R ¹ represents C _1-4 alkyl;
R ² represents C _1-6 alkyl substituted with one R ⁵ ;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A represents pyrazolyl optionally with one substituent selected from the group consisting of C _1-4 alkyl, and —C _1-4 alkyl-O—C _1-4 alkyl;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Wherein said C _5-7 cycloalkyl or 5-7 membered saturated heterocyclyl may be optionally substituted on one ring carbon atom with 1 or 2 C _1-4 alkyl substituents, or One ring carbon atom may be optionally substituted with oxo; and
Wherein the 5-7 membered saturated heterocyclyl may optionally be substituted on one or two ring N atoms with a C _1-6 alkyl substituent.
The compound according to [6] above, which is
[8] R ¹ represents C _1-4 alkyl;
R ² represents C _1-6 alkyl substituted with one R ⁵ ;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A represents pyrazolyl;
Ring B represents a 6-membered saturated heterocyclyl containing one heteroatom selected from O and N;
Wherein the 6-membered saturated heterocyclyl may be optionally substituted on one ring carbon atom with one C _1-4 alkyl substituent, which ring carbon atom is optionally substituted with oxo. In some cases; and
Wherein the 5-7 membered saturated heterocyclyl may optionally be substituted on one N atom with a C _1-6 alkyl substituent.
The compound according to [6] above, which is
[9] R ³ represents a fused bicyclic ring system selected from the structures below

The compound according to [8] above, which is characterized in that
[10] R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S, and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents; and
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system, where possible, is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2, or 3 one of _{C 1-4} alkyl is substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; one; _{C 1-4} alkyl substituted with one ^{R 13} C _1-4 alkyl substituted with R ¹⁸ ; -( C=O)-C _1-4 alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR. ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; and a substituent selected from the group consisting of C _2-6 alkenyl substituted with one R ^13. A group may be optionally substituted on one ring N atom, provided that Het ^1a or R ¹⁸ is directly bonded to the N atom, said Het ^1a or R ¹⁸ is N via a ring carbon atom. Shall be bound to an atom
The compound according to the above [1], wherein
[11] R ⁵ represents —NR ^6a R ^6b or —OR ⁷ ;
R ^6b represents hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or —C(═O)-C _1-4 alkyl;
R ⁷ represents hydrogen, C _1-4 alkyl, or —C _1-4 alkyl-NR ^8a R ^8b ;
R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; 1, 2 or 3 halo atoms. _{C 1-4} alkyl substituted; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2-6 alkenyl;} _{C 1-4} alkyl substituted with one ^{R 13;} And optionally a total of 1, 2 or 3 substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ and optionally substituted on a ring carbon atom. ;as well as
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic ring system is optionally substituted with C _1-6 alkyl; C _3-6 cycloalkyl; 1, 2 or 3 halo atoms. It is substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13;} 1,2 _{C 1-4} alkyl substituted or three -OH substituents,; _{C 1-4} alkyl that C _1-4 alkyl; C _2-6 alkenyl; and a substituent selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ optionally substituted on one ring N atom. There is;
Het ^1d represents a 4-7 membered monocyclic saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(=O) _p , and N;
Wherein the 4-7 membered monocyclic saturated heterocyclyl is selected from the group consisting of C _1-4 alkyl, C _3-6 cycloalkyl, and —OH and —O—C _1-4 alkyl, if possible. Optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _1-4 alkyl substituted with one substituent;
Here, monocyclic saturated heterocyclyl of said 4-7 membered, -OH, _{halo, C 1-4} alkyl, cyano, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1-4} alkyl ), and —N(C _1-4 alkyl) ₂ optionally substituted on one, two, or three ring C atoms with one or two substituents each independently selected from the group consisting of: There is;
R ¹³ represents —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, or Het ^1d .
The compound according to [10] above, which is
[12] R ¹ represents C _1-4 alkyl;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S and N;
Wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system may be optionally substituted on a ring carbon atom with a total of 1, 2, or 3 halo substituents; and
Wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system is C _1-4 alkyl substituted with 1, 2 or 3 —OH substituents when possible ; 1 R ¹³ Optionally substituted on one ring N atom with a substituent selected from the group consisting of C _1-4 alkyl substituted with
Het ^1d represents a 4-7 membered monocyclic saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(=O) _p , and N;
R ¹³ represents —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , or Het ^1d ;
R ^15a represents hydrogen or C _1-4 alkyl;
R ^15b represents C _1-4 alkyl
The compound according to [10] above, which is
[13] R ¹ represents C _1-4 alkyl;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused 9-membered bicyclic aromatic heterocyclic ring system containing one N atom;
Wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system may be optionally substituted on a ring carbon atom with a total of 1, 2, or 3 halo substituents; and
Wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system is C _1-4 alkyl substituted with 1, 2 or 3 —OH substituents when possible ; 1 R ¹³ Optionally substituted on one ring N atom with a substituent selected from the group consisting of C _1-4 alkyl substituted with
R ¹³ represents —O—C _1-4 alkyl or —C(═O)NR ^15a R ^15b ;
R ^15a represents hydrogen or C _1-4 alkyl;
R ^15b represents C _1-4 alkyl
The compound according to [10] above, which is
[14] R ¹ represents methyl; and
R ² represents methyl or —CH ₂ —OH
The compound according to any one of the above [1] to [13].
[15] The compound according to any one of the above [1] to [14], wherein Y represents CR ⁴ .
[16] The compound described in any one of [1] to [15] above, wherein R ⁴ represents hydrogen.
[17] The compound according to any one of the above [1] to [14], wherein Y represents N.
[18] The compound is compounds 21, 25, 32, 34, 35, 1b, 2b, 3b, 17b, 3c, and 8c, tautomers and stereoisomers thereof, and pharmaceutically acceptable addition salts. And a solvate, the compound according to the above [1].
[19] A pharmaceutical composition comprising the compound according to any one of [1] to [18] above and a pharmaceutically acceptable carrier or diluent.
[20] The compound according to any one of the above [1] to [18] for use as a drug.
[21] The compound according to any one of [1] to [18] above, which is used for preventing or treating cancer.
[22] The pharmaceutical composition according to the above [19], which is used for preventing or treating cancer.
[23] A method for treating or preventing a cell proliferative disease in a warm-blooded animal, wherein the warm-blooded animal is administered with an effective amount of the compound according to any one of [1] to [18] above. A method comprising the steps of:

Claims

A compound of formula (I), tautomers or stereoisomeric forms thereof, and pharmaceutically acceptable addition salts and solvates thereof,

In the formula,
R ¹ represents C _1-4 alkyl;
R ² _{is, C 1-6} represents alkyl, _{C 1-6} alkyl substituted with one ^{R 5,} or 1, 2, or _{C 1-6} alkyl substituted with 3 fluoro atoms;
Y represents CR ⁴ or N;
R ⁴ represents hydrogen or halo;
R ⁵ represents Het ^3a , —NR ^6a R ^6b , or —OR ⁷ ;
R ^6a represents hydrogen or C _1-4 alkyl;
R ^6b is hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; -C(=O)-C _1-4 alkyl; -C(=O)-Het ⁴ ; -S(=O) ₂ -C. _1-4 alkyl; -OH and -NR ^16a R ^16b, -C(=O)-C _1-4 alkyl substituted with one substituent selected from the group consisting of: -OH and -S(=O ) Represents C _1-4 alkyl substituted with one substituent selected from the group consisting of _2- C _1-4 alkyl;
R ⁷ is _{hydrogen, C 1-4} _{alkyl, -C 1-4} alkyl ^{^{^{-NR 8a R 8b, -C (=}}} O) -R 9, -S (= O) 2 -OH, -P (= O) 2 -OH, - (C = O) -CH (NH 2) -C 1-4 alkyl -Ar1, or _{-C 1-4} alkyl -Het ^3b;
R ^8a represents hydrogen or C _1-4 alkyl;
R ^8b represents hydrogen, C _1-4 alkyl, or C _3-6 cycloalkyl;
R ⁹ is _{C 1-6} alkyl, _or, -NH 2, -COOH, and _{C 1-6} alkyl substituted with one substituent selected from the group consisting of Het ⁶ represents;
R ^16a and R ^16b each independently represent hydrogen, C _1-4 alkyl, or C _3-6 cycloalkyl;
R ³ is
a) represents a fused bicyclic ring system of formula (1a-1) or (1a-2):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring A2 represents 2-oxo-1,2-dihydropyridin-3-yl;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) and (1a-2) is halo, cyano, oxo; _{-OH; C 1-6} alkyl; _{-O-C 1-4} ^{alkyl; -C (= O) -R 10} ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents;
Where Ring A2 is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2 or 3 C _1-4 alkyl substituted with 3 halo atoms, where possible; 1 , 2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2;} _{C 1-4} alkyl substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13} in and one _{C 2-6} substituents selected from the group consisting of alkenyl substituted with ^{R 13,} may be optionally substituted on the N atom; _-6 alkenyl However, ^{Het 1a} or ^{R 18} is When directly attached to the N atom of ring A2, said Het ^1a or R ¹⁸ shall be attached to the N atom via a ring carbon atom; and where ring B1 is C _1-6 when possible. Cycloalkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms; substituted with 1, 2 or 3 -OH substituents C _1-4 alkyl; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₈₎} _{-C 1-4} alkyl; one _{C 1-4} alkyl substituted with ^{R 13} -C ( =O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; And optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ ; provided that Het ^{When 1a} or R ¹⁸ is directly bonded to the N atom of ring B1, said Het ^1a or R ¹⁸ shall be bonded to the N atom via a ring carbon atom; or R ³ is
b) represents a fused bicyclic ring system of formula (2a-1):

Ring A _is selected from the group consisting of _{C 1-4} _{alkyl, -C 1-4} alkyl _{-O-C 1-4} alkyl, and 1,2, or _{C 1-4} alkyl substituted with three halo atoms Represents pyrazolyl optionally substituted with one substituent;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, the C _5-7 cycloalkyl or the 5-7 membered saturated heterocyclyl is C _1-4 alkyl, —C _1-4 alkyl-O—C _1-4 alkyl, and —C _1-4 alkyl-OH. Optionally substituted on one or two ring carbon atoms with one or two substituents each independently selected from the group consisting of, or one ring carbon atom optionally substituted with oxo. And wherein the 5-7 membered saturated heterocyclyl is C _1-6 alkyl; C _3-6 cycloalkyl; C _1-4 substituted with 1, 2 or 3 halo atoms. alkyl; 1,2, or 3 _{C 1-4} alkyl substituted with -OH substituents; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₃₎} _{-C 1-4} alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j is a substituent independently selected from the group consisting of 1 or 2 ring N atoms. It may be optionally substituted above; or R ³ is
c) represents a 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S, and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents; and wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system is C _{1- 6} alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms; substituted with 1, 2 or 3 -OH substituents C _1-4 alkyl; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₈₎} _{-C 1-4} alkyl; one _{C 1-4} alkyl substituted with ^{R 13} -C ( ═O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; And optionally substituted on one ring N atom with a substituent selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ ; provided that Het ^1a or R ¹⁸ is N When directly attached to an atom, said Het ^1a or R ¹⁸ shall be attached to the N atom via a ring carbon atom;
R ¹⁰ represents —OH, —O—C _1-4 alkyl, —NR ^11a R ^11b , or Het ² ;
R ¹⁸ represents a 5-membered aromatic ring containing 1, 2, or 3 N atoms;
Wherein the 5-membered aromatic ring may be optionally substituted with one substituent selected from the group consisting of C _1-4 alkyl and C _3-6 cycloalkyl;
Het ^1a , Het ^1c , and Het ^1d are each independently a 4- to 7-membered single or four-membered heteroatom containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N. A cyclic saturated heterocyclyl; or a fused ring, a spiro ring, and a bridged ring containing 1, 2, or 3 heteroatoms each independently selected from O, S, S(=O) _p , and N. Represents a 6-11 membered bicyclic saturated heterocyclyl including:
Wherein the 4 to 7 membered monocyclic saturated heterocyclyl or the 6 to 11 membered bicyclic saturated heterocyclyl is combined with C _1-4 alkyl, C _3-6 cycloalkyl, and —OH, if possible. A substituent independently selected from C _1-4 alkyl substituted with one substituent selected from the group consisting of —O—C _1-4 alkyl, 1, 2, or 3 ring N atoms. It may be optionally substituted above; and where said 4-7 membered monocyclic saturated heterocyclyl, or said 6-11 membered bicyclic saturated heterocyclyl is -OH, oxo, halo, C _{1 -4} alkyl, cyano, _-C (= _O) -C _1-4 alkyl, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1-4} alkyl), and -N _{(C 1-4} Optionally substituted on one, two, or three ring C atoms with one or two substituents each independently selected from the group consisting of alkyl) ₂ ;
Het ^1b , Het ^1e , Het ^1g , and Het ⁴ are each independently a 4-7 membered monocyclic group attached to the rest of the molecule of formula (I) through any available ring carbon atom. Represents saturated heterocyclyl, said Het ^1b , Het ^1e , Het ^1g , and Het ⁴ contain 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N. Are;
Wherein the 4-7 membered monocyclic saturated heterocyclyl is selected from the group consisting of C _1-4 alkyl, C _3-6 cycloalkyl, and —OH and —O—C _1-4 alkyl, if possible. Optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _1-4 alkyl substituted with one substituent; And the 4-7 membered monocyclic saturated heterocyclyl is -OH, halo, C _1-4 alkyl, cyano, -C(=O)-C _1-4 alkyl, -O-C _1-4 alkyl, 1 or 2 substituents each independently selected from the group consisting of —NH ₂ , —NH(C _1-4 alkyl), and —N(C _1-4 alkyl) ₂ , 1, 2, or 3 Optionally substituted on one ring C atom;
Het ² represents a heterocyclyl of formula (b-1):

(B-1) is an N-bonded 4-7 membered monocyclic saturated heterocyclyl optionally containing one additional heteroatom selected from O, S, S(═O) _p , and N, or 6 to 6 N-bonds, including fused, spiro, and bridged rings, optionally containing 1 or 2 additional heteroatoms each independently selected from O, S, S(=O) _p , and N. Represents an 11-membered bicyclic saturated heterocyclyl;
Wherein (b-1) comprises 1 or 2 additional N atoms, said 1 or 2 N atoms may be optionally substituted by C _1-4 alkyl; and where (b -1), halo, -OH, _{cyano, C 1-4} alkyl, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1-4} alkyl), - _{N (C 1-4} alkyl) Optionally substituted on one, two, or three ring C atoms with 1 or 2 substituents each independently selected from the group consisting of ₂ , and C _1-4 alkyl-OH;
R ^11b is hydrogen; Het ^1e ; C _1-4 alkyl; C _1-4 alkyl-Het ⁵ ; halo, —OH, and —O—C _1-4 alkyl each independently selected from the group consisting of 1, 2, or 3 _{C 1-4} alkyl substituted with a _substituent; each independently selected from or halo, -OH, and _{-O-C 1-4} group consisting of alkyl; _{C 3-6} cycloalkyl Represents C _3-6 cycloalkyl substituted with 1, 2 or 3 substituents;
R ¹³ is —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, Het ^1d , —S(═O) ₂ —C _{1 -4} alkyl, -S(=O)(=N-R ^20c )-C _1-4 alkyl, or -C(=O)-Het ^1f ;
R ¹² is —OH, —O—C _1-4 alkyl, —NR ^14a R ^14b , —C(═O)NR ^14c R ^14d , —S(═O) ₂ —C _1-4 alkyl, —S(= O) (=NR ^20b )-C _1-4 alkyl, C _3-6 cycloalkyl, Ar ² or Het ^1c ;
Ar ¹ represents phenyl optionally substituted with one hydroxy;
Ar ² represents phenyl optionally substituted with one C _1-4 alkyl;
Het ^3a , Het ^3b , Het ⁵ , Het ⁶ , and Het ^1f each independently represent a heterocyclyl of formula (c-1):

(C-1) represents an N-bonded 4 to 7 membered monocyclic saturated heterocyclyl optionally containing one additional heteroatom selected from O, S, S(=O) _p , and N;
Here, when (c-1) contains one additional N atom, the additional N atom may be optionally substituted with C _1-4 alkyl or C _3-6 cycloalkyl; and where: (C-1) is 1 or 2 substituents each independently selected from the group consisting of halo, C _1-4 alkyl, and C _3-6 cycloalkyl, and on 1 or 2 ring C atoms. May be replaced at will;
R ^11a , R ^14a , R ^14c , R ^14g , R ¹⁴ⁱ , R ^14k , R ^15a , R ^17a , and R ^19a each independently represent hydrogen or C _1-4 alkyl;
R ^14b , R ^14d , R ^14h , R ^14j , R ^14l , R ^15b , R ^17b , and R ^19b are each independently hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or halo, −. OH, and _{-O-C 1-4} represents _{C 1-4} alkyl substituted with one substituent selected from the group consisting of alkyl;
R ^20a , R ^20b , and R ^20c are each independently selected from the group consisting of hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or —OH and —O—C _1-4 alkyl. Represents C _1-4 alkyl substituted with one substituent;
A compound characterized in that p represents 1 or 2.

R ³ represents a fused bicyclic ring system of formula (1a-1) or (1a-2):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring A2 represents 2-oxo-1,2-dihydropyridin-3-yl;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) and (1a-2) is halo, cyano, oxo; _{-OH; C 1-6} alkyl; _{-O-C 1-4} ^{alkyl; -C (= O) -R 10} ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents;
Where Ring A2 is C _1-6 alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; 1, 2 or 3 C _1-4 alkyl substituted with 3 halo atoms, where possible; 1 , 2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2;} _{C 1-4} alkyl substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13} in and one _{C 2-6} substituents selected from the group consisting of alkenyl substituted with ^{R 13,} may be optionally substituted on the N atom; _-6 alkenyl However, ^{Het 1a} or ^{R 18} is When directly attached to the N atom of ring A2, said Het ^1a or R ¹⁸ shall be attached to the N atom via a ring carbon atom; and where ring B1 is C _1-6 when possible. Cycloalkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms; substituted with 1, 2 or 3 -OH substituents C _1-4 alkyl; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₈₎} _{-C 1-4} alkyl; one _{C 1-4} alkyl substituted with ^{R 13} -C ( ═O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; And optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ ; provided that Het If ^1a or the R ¹⁸ is directly bonded to the N atom of the ring B1, the Het ^1a or R ¹⁸ is as defined in claim 1, characterized in that shall be attached to the N atom via a ring carbon atom Compound.

R ⁵ represents -OR ^7;
R ⁷ is _{hydrogen, C 1-4} _{alkyl, -C 1-4} alkyl ^{^{^{-NR 8a R 8b, -C (=}}} O) -R 9, - (C = O) -CH (NH 2) -, or _{C 1 -4} alkyl-Ar ¹ ;
R ⁹ is _{C 1-6} alkyl, or represents _{C 1-6} alkyl substituted with one substituent selected from the group consisting of -NH ₂ and -COOH;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(═O) _p , and N;
Here, (1a-1) is halo; cyano; oxo; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S(=O) ₂ -C. _1-4 alkyl; 1,2, or _{-O-C 1-4} alkyl substituted with three halo atoms; _{-O-C 1-4} alkyl ^-R _{12; C 3-6} cycloalkyl; -O-C _3-6 _{cycloalkyl; -NH-C (= O)} -C 1-4 ^alkyl; -NR ^17a R 17b; 1,2, or _{C 1-4} alkyl is substituted with three halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R _13;} _{C 2-6} alkenyl; _{C 2-6} substituted with and one ^{R 13} It may be optionally substituted on a ring carbon atom with a total of 1, 2 or 3 substituents each independently selected from the group consisting of alkenyl; and where ring B 1 is, where possible, _{C 1} is substituted with 1, 2, or 3 -OH substituents; C _1-6 _{cycloalkyl; C 3-6} cycloalkyl; 1,2, or 3 _{C 1-4} alkyl substituted with halo atoms _-4 alkyl; C _1-4 alkyl substituted with one R ¹³ ; -(C=O)-C _1-4 alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C. consisting _{C 2-6} alkenyl substituted with and one ^{R 13;} _1-4 alkyl ^{^{-NR 14i R 14j; -C (=}} O) -C (= O) -NR 14k R 14l; C 2-6 alkenyl Substituents independently selected from the group optionally substituted on one or two ring N atoms;
R ¹⁰ represents —OH, —O—C _1-4 alkyl, or —NR ^11a R ^11b ;
R ^11b is hydrogen; C _1-4 alkyl; C substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, —OH, and —O—C _1-4 alkyl. _1-4 alkyl; C _3-6 cycloalkyl; or substituted with 1, 2, or 3 substituents each independently selected from the group consisting of halo, —OH, and —O—C _1-4 alkyl. Represents C _3-6 cycloalkyl;
R ¹³ is —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, or —S(═O) ₂ —C _1-4 alkyl. Represents;
R ¹² is —OH, —O—C _1-4 alkyl, —NR ^14a R ^14b , —C(═O)NR ^14c R ^14d , —S(═O) ₂ —C _1-4 alkyl, C _3-6. A compound according to claim 1 or 2, characterized in that it represents cycloalkyl or Ar ² .

R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents a 6-membered aromatic heterocycle containing 1 or 2 N atoms;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, (1a-1) is halo; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -O-C _1-4 alkyl-R ¹² ;-. NR ^17a R ^17b; 1, 2, or 3 _{C 1-4} alkyl substituted with -OH substituents; _{C 1-4} alkyl substituted with one ^{R _13;} _{C 2-6} alkenyl; and one R It may be optionally substituted on a ring carbon atom with a total of 1, 2, or 3 substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with ¹³ ; , Ring B1 is C _1-6 cycloalkyl when possible; C _1-4 alkyl substituted with one R ¹³ ; -(C=O)-C _1-4 alkyl; -C(=O)- C _1-4 alkyl ^-NR 14i ^{R 14j;} and ^{-C (= O) -C (=} O) -NR 14k R with a substituent selected independently from the group consisting of ^14l, 1 or 2 ring N Optionally substituted on an atom;
R ¹⁰ represents -NR ^11a R ^11b ;
R ^11b represents C _1-4 alkyl;
R ¹³ represents —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , or C _3-6 cycloalkyl;
R ¹² represents C _3-6 cycloalkyl;
R ^11a , R ¹⁴ⁱ , R ^14k , R ^15a , and R ^17a each independently represent hydrogen or C _1-4 alkyl;
The compound according to claim 1 or 2, wherein R ^14j , R ¹⁴¹ , R ^15b , and R ^17b each independently represent hydrogen or C _1-4 alkyl.

R ² represents C _1-6 alkyl substituted with one R ⁵ ;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (1a-1):

Ring A1 represents phenyl or a 6-membered aromatic heterocycle containing one N atom;
Ring B1 represents a 4-7 membered saturated heterocyclyl containing one heteroatom selected from O and N;
Here, (1a-1) is each a group consisting of —O—C _1-4 alkyl; —O—C _1-4 alkyl-R ¹² ; and C _1-4 alkyl substituted with one R ^13. It may optionally be substituted on a ring carbon atom with a total of 1, 2 or 3 independently selected substituents; and where Ring B is C _1-6 alkyl substituted where possible. A group may be optionally substituted on one N atom;
R ¹³ represents C _3-6 cycloalkyl;
The compound according to claim 1 or 2, characterized in that R ¹² represents C _3-6 cycloalkyl.

R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A _is selected from the group consisting of _{C 1-4} _{alkyl, -C 1-4} alkyl _{-O-C 1-4} alkyl, and 1,2, or _{C 1-4} alkyl substituted with three halo atoms Represents pyrazolyl optionally substituted with one substituent;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Here, the C _5-7 cycloalkyl or the 5-7 membered saturated heterocyclyl is C _1-4 alkyl, —C _1-4 alkyl-O—C _1-4 alkyl, and —C _1-4 alkyl-OH. Optionally substituted on one or two ring carbon atoms with one or two substituents each independently selected from the group consisting of, or one ring carbon atom optionally substituted with oxo. And wherein the 5-7 membered saturated heterocyclyl is C _1-6 alkyl; C _3-6 cycloalkyl; C _1-4 substituted with 1, 2 or 3 halo atoms. alkyl; 1,2, or 3 _{C 1-4} alkyl substituted with -OH substituents; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₃₎} _{-C 1-4} alkyl; -C(=O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j is a substituent independently selected from the group consisting of 1 or 2 ring N atoms. The compound of claim 1, wherein the compound may be optionally substituted above.

R ¹ represents C _1-4 alkyl;
R ² represents C _1-6 alkyl substituted with one R ⁵ ;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A represents pyrazolyl optionally with one substituent selected from the group consisting of C _1-4 alkyl, and —C _1-4 alkyl-O—C _1-4 alkyl;
Ring B represents C _5-7 cycloalkyl or a 5-7 membered saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O and N;
Wherein said C _5-7 cycloalkyl or 5-7 membered saturated heterocyclyl may be optionally substituted on one ring carbon atom with 1 or 2 C _1-4 alkyl substituents, or One ring carbon atom may be optionally substituted with oxo; and wherein said 5-7 membered saturated heterocyclyl is a C _1-6 alkyl substituent, optionally on one or two ring N atoms. The compound according to claim 6, wherein the compound may be substituted with.

R ¹ represents C _1-4 alkyl;
R ² represents C _1-6 alkyl substituted with one R ⁵ ;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused bicyclic ring system of formula (2a-1):

Ring A represents pyrazolyl;
Ring B represents a 6-membered saturated heterocyclyl containing one heteroatom selected from O and N;
Wherein the 6-membered saturated heterocyclyl may be optionally substituted on one ring carbon atom with one C _1-4 alkyl substituent, wherein one ring carbon atom is optionally substituted with oxo. And wherein the 5-7 membered saturated heterocyclyl may optionally be substituted on one N atom with a C _1-6 alkyl substituent. The described compound.

R ³ represents a fused bicyclic ring system selected from the following structures

The compound according to claim 8, characterized in that

R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; -C(=O)-R ¹⁰ ; -S ₍₌ O) _{2 -C 1-4} ^{alkyl; -S (= O) (=} N-R 20a) -C 1-4 alkyl; substituted with 1, 2, or 3 halo atoms -O- C _1-4 alkyl; -O-C _1-4 alkyl-R ¹² ; C _3-6 cycloalkyl; -O-C _3-6 cycloalkyl; Het ^1a ; -O-Het ^1b ; R ¹⁸ ; -P( ═O)-(C _1-4 alkyl) ₂ ; —NH—C(═O)—C _1-4 alkyl; —NH—C(═O)—Het ^1g ; —NR ^17a R ^17b ; or 3 _{C 1-4} alkyl substituted with halo atoms; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 1-4} alkyl substituted with one ^{R 13;} _{C 2-6 alkenyl;} and one total are each independently selected from the group consisting of _{C 2-6} alkenyl substituted with ^{R 13} 1,2, _{C 1-4} alkyl substituted with one ^{R 18} Or optionally substituted on a ring carbon atom with three substituents; and wherein said fused 6-11 membered bicyclic aromatic heterocyclic ring system is C _{1- 6} alkyl; C _3-6 cycloalkyl; Het ^1a ; R ¹⁸ ; C _1-4 alkyl substituted with 1, 2 or 3 halo atoms; substituted with 1, 2 or 3 -OH substituents C _1-4 alkyl; _{C 1-4} alkyl ;-( C = O is substituted with one ^{R ₁₈₎} _{-C 1-4} alkyl; one _{C 1-4} alkyl substituted with ^{R 13} -C ( =O)NR ^14g R ^14h ; -C(=O)-C _1-4 alkyl-NR ¹⁴ⁱ R ^14j ; -C(=O)-C(=O)-NR ^14k R ^14l ; C _2-6 alkenyl; And optionally substituted on one ring N atom with a substituent selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ ; provided that Het ^1a or R ¹⁸ is N A compound according to claim 1, characterized in that, when directly attached to an atom, the Het ^1a or R ¹⁸ is attached to the N atom via a ring carbon atom.

R ⁵ represents —NR ^6a R ^6b or —OR ⁷ ;
R ^6b represents hydrogen; C _1-4 alkyl; C _3-6 cycloalkyl; or —C(═O)-C _1-4 alkyl;
R ⁷ represents hydrogen, C _1-4 alkyl, or —C _1-4 alkyl-NR ^8a R ^8b ;
R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic system is halo; cyano; C _1-6 alkyl; -O-C _1-4 alkyl; 1, 2, or 3 halo atoms. _{C 1-4} alkyl substituted; 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; _{C 2-6 alkenyl;} _{C 1-4} alkyl substituted with one ^{R 13;} And optionally a total of 1, 2, or 3 substituents each independently selected from the group consisting of C _2-6 alkenyl substituted with one R ¹³ and optionally substituted on a ring carbon atom. And where the fused 6-11 membered bicyclic aromatic heterocyclic ring system is, where possible, C _1-6 alkyl; C _3-6 cycloalkyl; 1, 2, or 3 halo atoms. substituted with one ^{R 18;} _{C 1-4} alkyl substituted with one ^{R 13;} 1,2 _{C 1-4} alkyl or substituted with three -OH substituents,; _{C 1-4} alkyl substituted _{C 2-6 alkenyl;;} _{C 1-4} alkyl which is a substituent selected from the group consisting of and _{C 2-6} alkenyl substituted with one ^{R 13,} optionally substituted on one ring N atoms May be;
Het ^1d represents a 4-7 membered monocyclic saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(=O) _p , and N;
Wherein the 4-7 membered monocyclic saturated heterocyclyl is selected from the group consisting of C _1-4 alkyl, C _3-6 cycloalkyl, and —OH and —O—C _1-4 alkyl, if possible. Optionally substituted on one or two ring N atoms with substituents each independently selected from the group consisting of C _1-4 alkyl substituted with one substituent; in, monocyclic saturated heterocyclyl of said 4-7 membered, -OH, _{halo, C 1-4} alkyl, cyano, _{-O-C 1-4} _alkyl, -NH _2, -NH _{(C 1-4} alkyl) , And —N(C _1-4 alkyl) ₂ each independently having 1 or 2 substituents independently selected from the group consisting of 1, 2 or 3 ring C atoms. Yes;
R ¹³ represents —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , —NR ^19a R ^19b , C _3-6 cycloalkyl, or Het ^1d. The described compound.

R ¹ represents C _1-4 alkyl;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused 6-11 membered bicyclic aromatic heterocyclic ring system containing 1 or 2 heteroatoms each independently selected from O, S and N;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic ring system may be optionally substituted on a ring carbon atom with a total of 1, 2, or 3 halo substituents; and here in bicyclic heteroaromatic ring system of 6 to 11 membered engaged the reduced, if possible, 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; one ^{R 13} Substituents selected from the group consisting of substituted C _1-4 alkyl, optionally substituted on one ring N atom;
Het ^1d represents a 4-7 membered monocyclic saturated heterocyclyl containing 1 or 2 heteroatoms each independently selected from O, S, S(=O) _p , and N;
R ¹³ represents —O—C _1-4 alkyl, —C(═O)NR ^15a R ^15b , or Het ^1d ;
R ^15a represents hydrogen or C _1-4 alkyl;
The compound according to claim 10, wherein R ^15b represents C _1-4 alkyl.

R ¹ represents C _1-4 alkyl;
R ⁵ represents -OR ^7;
R ⁷ represents hydrogen;
R ³ represents a fused 9-membered bicyclic aromatic heterocyclic ring system containing one N atom;
Wherein the fused 6-11 membered bicyclic aromatic heterocyclic ring system may be optionally substituted on a ring carbon atom with a total of 1, 2, or 3 halo substituents; and here in bicyclic heteroaromatic ring system of 6 to 11 membered engaged the reduced, if possible, 1,2, or _{C 1-4} alkyl is substituted with three -OH substituents; one ^{R 13} Substituents selected from the group consisting of substituted C _1-4 alkyl, optionally substituted on one ring N atom;
R ¹³ represents -O-C _1-4 alkyl or -C(=O)NR ^15a R ^15b ;
R ^15a represents hydrogen or C _1-4 alkyl;
The compound according to claim 10, wherein R ^15b represents C _1-4 alkyl.

R ¹ represents methyl; A compound according to and ^{R 2} any one of claims 1 to 13, characterized in that represents a methyl or _-CH 2 -OH.

A compound according to Y represents CR ^4, any one of claims 1 to 14, wherein the.

A compound according to R ⁴ represents hydrogen, any one of claims 1 to 15, characterized in that.

The compound according to any one of claims 1 to 14, characterized in that Y represents N.

The compounds include compounds 21, 25, 32, 34, 35, 1b, 2b, 3b, 17b, 3c, and 8c, tautomers and stereoisomers thereof, and pharmaceutically acceptable addition salts and solvates. The compound according to claim 1, wherein the compound is selected from the group consisting of:

A pharmaceutical composition comprising a compound according to any one of claims 1 to 18 and a pharmaceutically acceptable carrier or diluent.

A pharmaceutical composition comprising a compound according to any one of claims 1 to 18 for use as a medicament .

A pharmaceutical composition comprising a compound according to any one of claims 1 to 18 for use in the prevention or treatment of cancer.

A pharmaceutical composition for treating or preventing a warm-blooded animal a cell proliferative disease, including a compound according to any one of claims 1 to 18 in effective amounts, pharmaceutical compositions.